U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 551 - 560 of 609 results

PD-153035 is a potent and selective ATP-competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR. PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced by EGF in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells. PD153035 shows dose-dependent growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines (A431, Difi, DU145, MDA-MB-468, and ME180) and in nasopharyngeal carcinoma (NPC) cell lines (NPC-TW01, NPC-TW04, and HONE1). Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluorouracil in NPCTW04 cells. PD153035 abolishes COX-2 expression induced by the PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon cancer cells. In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg i.p. inhibit EGF receptor tyrosine kinase activity. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice.
Geraniol is a dietary monoterpene alcohol that is found in the essential oils of aromatic plants. To date, experimental evidence supports the therapeutic or preventive effects of geraniol on different types of cancer, such as breast, lung, colon, prostate, pancreatic, and hepatic cancer, and has revealed the mechanistic basis for its pharmacological actions. In addition, geraniol sensitizes tumor cells to commonly used chemotherapy agents. Geraniol controls a variety of signaling molecules and pathways that represent tumor hallmarks; these actions of geraniol constrain the ability of tumor cells to acquire adaptive resistance against anticancer drugs. It has been shown that geraniol inhibits HMG-CoA reductase in most types of tumor cells, which raises the possibility that the reduced prenylation of small G-proteins, such as Ras or RhoA, accounts for the antitumor effects of geraniol. In addition to its use in various commercial products, including cosmetics and fine fragrances, geraniol exerts a broad spectrum of pharmacological activities, such as anti-microbial, anti-inflammatory, anti-oxidant, anti-ulcer and neuroprotective activities. Geraniol is classified into the generally recognized-as-safe (GRAS) category by the Flavor and Extract Manufacturers Association (FEMA) and the Food and Drug Administration (FDA) of the United States.
Status:
US Previously Marketed
First approved in 1997

Class (Stereo):
CHEMICAL (ACHIRAL)


Mangafodipir (sold under the brand name Teslascan as mangafodipir trisodium) is a contrast agent delivered intravenously to enhance contrast in magnetic resonance imaging (MRI) of the liver. Mangafodipir is a manganese (Mn2+) chelate with the ligand fodipir (dipyridoxyl diphosphate or DPDP). Mangafodipir trisodium is metabolised (dephosphorylated) and partially transmetallated (manganese exchanged for zinc) after intravenous administration. Manganese that is released from mangafodipir is taken up by hepatocytes thereby increasing the SI of normal liver tissue. This may result in an improvement of the detection of liver metastases, which usually have no hepatocytes. The metabolites of fodipir are renally excreted, whilst the biliary route mainly excretes manganese. Mangafodipir was withdrawn from the US market in 2003 and the European market in 2012.
Anethole is a flavoring agent in foods and beverages; in perfumery, particularly for soap and dentifrices. The more abundant isomer, and the one preferred for use, is the trans- or E isomer. It is distinctly sweet, measuring 13 times sweeter than sugar. Anethole has potent antimicrobial properties, against bacteria, yeast, and fungi. Anethole also has nematicidal activity and is a promising insecticide. Several essential oils consisting mostly of anethole have insecticidal action. Anethole has estrogenic activity. It is slightly toxic and may act as an irritant in large quantities.
Status:
US Previously Marketed
Source:
Reneal by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Reneal by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phytic acid is a major phosphorus storage compound of most seeds and cereal grains. It has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron. Phytic acid is also considered to be a natural antioxidant and is suggested to have potential functions of reducing lipid peroxidation and as a preservative in foods. Clathrin-associated adaprot complex AP-2 has it been suggested may act as one of the receptor sites for Phytic acid. Both in vivo and in vitro experiments have demonstrated striking anticancer (preventive as well as therapeutic) effects of Phytic acid.
Status:
US Previously Marketed
Source:
Reneal by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Reneal by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phytic acid is a major phosphorus storage compound of most seeds and cereal grains. It has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron. Phytic acid is also considered to be a natural antioxidant and is suggested to have potential functions of reducing lipid peroxidation and as a preservative in foods. Clathrin-associated adaprot complex AP-2 has it been suggested may act as one of the receptor sites for Phytic acid. Both in vivo and in vitro experiments have demonstrated striking anticancer (preventive as well as therapeutic) effects of Phytic acid.
Status:
US Previously Marketed
Source:
Reneal by Squibb
(1962)
Source URL:
First approved in 1962
Source:
Reneal by Squibb
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Phytic acid is a major phosphorus storage compound of most seeds and cereal grains. It has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron. Phytic acid is also considered to be a natural antioxidant and is suggested to have potential functions of reducing lipid peroxidation and as a preservative in foods. Clathrin-associated adaprot complex AP-2 has it been suggested may act as one of the receptor sites for Phytic acid. Both in vivo and in vitro experiments have demonstrated striking anticancer (preventive as well as therapeutic) effects of Phytic acid.
Status:
US Previously Marketed
Source:
Oralator by Smith Kline & French
(1946)
Source URL:
First approved in 1946
Source:
Oralator by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)


Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Octodrine, has a history of use as a pharmaceutical drug. It was originally developed in the United States as an aerosolized treatment for bronchitis, laryngitis and other conditions Initially approved by the FDA in 1946 as Eskay’s Oralator, this inhaler appeared only in the 1949 edition of the Physicians’ Desk Reference. Octodrine was combined with several other medications, including theophylline, 3-octopamine, and adenosine, in multi-ingredient tablets sold between the early 1960s through the mid-2000s under the trade names Ambredin, Ordinal, Ordinal Retard and Ordinal Forte. Some proponents say octodrine is a safer alternative to other stimulants like ephedra and Dimethylamylamine (DMAA), but there is no scientific information to support this claim. Originally developed in the early 1950’s as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.
Status:
US Previously Marketed
Source:
Oralator by Smith Kline & French
(1946)
Source URL:
First approved in 1946
Source:
Oralator by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Octodrine, has a history of use as a pharmaceutical drug. It was originally developed in the United States as an aerosolized treatment for bronchitis, laryngitis and other conditions Initially approved by the FDA in 1946 as Eskay’s Oralator, this inhaler appeared only in the 1949 edition of the Physicians’ Desk Reference. Octodrine was combined with several other medications, including theophylline, 3-octopamine, and adenosine, in multi-ingredient tablets sold between the early 1960s through the mid-2000s under the trade names Ambredin, Ordinal, Ordinal Retard and Ordinal Forte. Some proponents say octodrine is a safer alternative to other stimulants like ephedra and Dimethylamylamine (DMAA), but there is no scientific information to support this claim. Originally developed in the early 1950’s as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.
Status:
US Previously Marketed
Source:
Oralator by Smith Kline & French
(1946)
Source URL:
First approved in 1946
Source:
Oralator by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Octodrine, has a history of use as a pharmaceutical drug. It was originally developed in the United States as an aerosolized treatment for bronchitis, laryngitis and other conditions Initially approved by the FDA in 1946 as Eskay’s Oralator, this inhaler appeared only in the 1949 edition of the Physicians’ Desk Reference. Octodrine was combined with several other medications, including theophylline, 3-octopamine, and adenosine, in multi-ingredient tablets sold between the early 1960s through the mid-2000s under the trade names Ambredin, Ordinal, Ordinal Retard and Ordinal Forte. Some proponents say octodrine is a safer alternative to other stimulants like ephedra and Dimethylamylamine (DMAA), but there is no scientific information to support this claim. Originally developed in the early 1950’s as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.

Showing 551 - 560 of 609 results